Table 3.
Kinase inhibitors/activators for autophagy induction.
| Name | Mechanism | Cell line | Disease | Clinical status | Ref. |
|---|---|---|---|---|---|
| GDC-0941 | PI3K inhibition | MCF-7, T47D and ZR75-1 cells | ER+ breast cancer | Phase 1 | 80 |
| Taselisib | PI3K inhibition | Human KPL-4 breast cancer cell | Advanced solid tumors | Phase 3 | 81 |
| PX-866 | PI3K inhibition | LNZ308 and LN229 cells | Glioblastoma | Phase 1 | 82 |
| PKI-587 | PI3K/mTOR inhibition | A431-CR and FaDu-CR cells | Breast cancer, non-small cell lung cancer, ovarian cancer, etc. | Phase 1/2 | 83 |
| BEZ235 | PI3K/mTOR inhibition | 786-0 and Caki-1 cells | Metastatic renal cell carcinoma | Phase 1 | 84, 85 |
| PF-04691502 | PI3K/mTOR inhibition | A549 cells | Non-small cell lung cancer | Phase 1 | 86 |
| Perifosine | AKT inhibition | T98G and U373MG cells | Glioblastoma, anaplastic astrocytoma, mixed glioma, etc. | Phase 2 | 87, 88 |
| MK2206 | AKT inhibition | UL cells | Colon mucinous adenocarcinoma, colon signet ring cell adenocarcinoma, rectal mucinous adenocarcinoma, etc. | Phase 2 | 89 |
| BI-69A11 | AKT inhibition | HT-29 cell | – | – | 90 |
| Metformin | AMPK activation | EC109 cells | Diabetes mellitus type 2 | Phase 4 | 91 |
| Salicylate | AMPK activation | HEK-293 cells | – | – | 31 |
| Hernandezine | AMPK activation | HeLa cells | – | – | 92 |
| Simvastatin | AMPK activation | Mouse coronary arterial myocytes | Coronary arterial myocytes | Phase 1/2 | 93 |
| A-769662 | AMPK activation | U373 cells | – | – | 94 |
| Rapamycin | mTOC1 inhibition | SK-N-SH and SH-SY5Y cells | Primitive neurotodermal tumor and mast cell leukemia | – | 95, 96 |
| AZD8055 | mTOC1 inhibition | H838 and A549 cells | Glioblastoma multiforme, advanced hepatocellular carcinoma, advanced solid malignancies, etc. | Phase 1 | 97 |
| PP242 | mTOC1 inhibition | HeLa cells | – | – | 98 |
| RapaLink-1 | mTOC1 inhibition | MCF-7, RR1 and RR2 cells | – | – | 99 |
| LYN-1604 | ULK1 activation | MDA-MB-231 cells | Triple negative breast cancer | – | 100 |
| BL-918 | ULK1 activation | SH-SY5Y cells | Parkinson's disease | 101 | |
| JNK-IN-8 | JNK1 inhibition | Primary hepatocytes and primary epithelial cells | – | – | 102 |
| HJ-PI01 | PIM2 inhibition | MDA-MB-231 cells | – | – | 103 |
| SMI-4a | PIM2 inhibition | A375 and G361 cells | – | – | 104 |
| SGI-1776 | PIM2 inhibition | MM.1S cells | Relapsed/refractory leukemias | Phase 1 | 105 |
| AZD1208 | PIM2 inhibition | Primary chronic lymphocytic leukemia cells | Primary chronic lymphocytic leukemia | Phase 1 | 106 |
| SB216763 | GSK3β inhibition | Human pancreatic cancer cells | – | – | 107 |
| CHIR99021 | GSK3 inhibition | Human pancreatic cancer cells | – | – | 108 |
| TDZD8 | GSK3β inhibition | PC-3 cells | – | – | 109 |
| 9-ING-41 | GSK3 inhibition | PC-3 cells | Lymphoma pancreatic cancer | Phase 1/2 | 110 |
| SCH7 72984 | ERK1 inhibition | HPAC and PANC-1 cells | – | – | 111 |
| BVD-523 | ERK1 inhibition | HPAC and PANC-1 cells | Advanced solid tumors | Phase 1/2 | 111, 112 |
| GDC-0994 | ERK1 inhibition | Epithelial Caco-2 and HT-29 cells | – | – | 113 |
| LRRK2-IN-1 | LRRK2 inhibition | H4 astroglioma cells | – | – | 76 |
| GSK2578215A | LRRK2 inhibition | SH-SY5Y cells | – | – | 114 |
| SB202190 | MAPK inhibition | HT29 cells | – | – | 115 |
| SB203580 | MAPK inhibition | HCC cells | – | – | 116 |
– Not applicable.